AU2012350751B2 - Substituted triazolopyridines and their use as TTK inhibitors - Google Patents
Substituted triazolopyridines and their use as TTK inhibitors Download PDFInfo
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- AU2012350751B2 AU2012350751B2 AU2012350751A AU2012350751A AU2012350751B2 AU 2012350751 B2 AU2012350751 B2 AU 2012350751B2 AU 2012350751 A AU2012350751 A AU 2012350751A AU 2012350751 A AU2012350751 A AU 2012350751A AU 2012350751 B2 AU2012350751 B2 AU 2012350751B2
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- 239000003112 inhibitor Substances 0.000 title description 12
- 150000008523 triazolopyridines Chemical class 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims abstract description 548
- 239000000203 mixture Substances 0.000 claims description 255
- -1 methyl- Chemical group 0.000 claims description 238
- 238000000034 method Methods 0.000 claims description 140
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 85
- 150000003839 salts Chemical class 0.000 claims description 75
- 125000005843 halogen group Chemical group 0.000 claims description 71
- 206010028980 Neoplasm Diseases 0.000 claims description 69
- 238000002360 preparation method Methods 0.000 claims description 60
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 56
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 53
- 239000012453 solvate Substances 0.000 claims description 49
- 150000001204 N-oxides Chemical class 0.000 claims description 42
- 238000011282 treatment Methods 0.000 claims description 41
- 201000010099 disease Diseases 0.000 claims description 34
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 32
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 29
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 238000005859 coupling reaction Methods 0.000 claims description 26
- 150000002148 esters Chemical class 0.000 claims description 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 23
- 239000003795 chemical substances by application Substances 0.000 claims description 22
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
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- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- IHIXIJGXTJIKRB-UHFFFAOYSA-N trisodium vanadate Chemical compound [Na+].[Na+].[Na+].[O-][V]([O-])([O-])=O IHIXIJGXTJIKRB-UHFFFAOYSA-N 0.000 description 1
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- 229910052722 tritium Inorganic materials 0.000 description 1
- GPRLSGONYQIRFK-MNYXATJNSA-N triton Chemical compound [3H+] GPRLSGONYQIRFK-MNYXATJNSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Molecular Biology (AREA)
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cosmetics (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193011 | 2011-12-12 | ||
| EP11193011.1 | 2011-12-12 | ||
| PCT/EP2012/074978 WO2013087579A1 (fr) | 2011-12-12 | 2012-12-10 | Triazolopyridines substituées et leur utilisation à titre d'inhibiteurs de ttk |
Publications (2)
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| AU2012350751A1 AU2012350751A1 (en) | 2014-06-26 |
| AU2012350751B2 true AU2012350751B2 (en) | 2017-07-06 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2012350751A Ceased AU2012350751B2 (en) | 2011-12-12 | 2012-12-10 | Substituted triazolopyridines and their use as TTK inhibitors |
Country Status (39)
| Country | Link |
|---|---|
| US (1) | US9663510B2 (fr) |
| EP (1) | EP2791136B1 (fr) |
| JP (1) | JP6181664B2 (fr) |
| KR (1) | KR20140105552A (fr) |
| CN (1) | CN104114552B (fr) |
| AP (1) | AP4017A (fr) |
| AR (1) | AR089143A1 (fr) |
| AU (1) | AU2012350751B2 (fr) |
| BR (1) | BR112014014184A2 (fr) |
| CA (1) | CA2858683A1 (fr) |
| CL (1) | CL2014001546A1 (fr) |
| CO (1) | CO6980657A2 (fr) |
| CR (1) | CR20140275A (fr) |
| CU (1) | CU20140068A7 (fr) |
| CY (1) | CY1116958T1 (fr) |
| DK (1) | DK2791136T3 (fr) |
| DO (1) | DOP2014000133A (fr) |
| EC (1) | ECSP14004812A (fr) |
| ES (1) | ES2550677T3 (fr) |
| GT (1) | GT201400111A (fr) |
| HR (1) | HRP20151103T1 (fr) |
| HU (1) | HUE025937T2 (fr) |
| IL (1) | IL232930A (fr) |
| JO (1) | JO3111B1 (fr) |
| MA (1) | MA35826B1 (fr) |
| MX (1) | MX2014007057A (fr) |
| PE (1) | PE20141597A1 (fr) |
| PH (1) | PH12014501319A1 (fr) |
| PL (1) | PL2791136T3 (fr) |
| PT (1) | PT2791136E (fr) |
| RS (1) | RS54288B1 (fr) |
| RU (1) | RU2632464C1 (fr) |
| SG (1) | SG11201402820SA (fr) |
| SI (1) | SI2791136T1 (fr) |
| TN (1) | TN2014000254A1 (fr) |
| UA (1) | UA112096C2 (fr) |
| UY (1) | UY34515A (fr) |
| WO (1) | WO2013087579A1 (fr) |
| ZA (1) | ZA201404031B (fr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EA027544B1 (ru) * | 2012-07-10 | 2017-08-31 | Байер Фарма Акциенгезельшафт | Способ получения замещенных триазолопиридинов |
| WO2014020041A1 (fr) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinaisons pour le traitement du cancer |
| WO2014020043A1 (fr) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinaisons pour le traitement du cancer |
| AR096469A1 (es) * | 2013-06-06 | 2015-12-30 | Bayer Pharma AG | Composiciones farmacéuticas que comprenden compuestos del tipo triazolpiridinas |
| HUE033131T2 (en) * | 2013-06-11 | 2017-11-28 | Bayer Pharma AG | Derivatives of substituted triazolopyridines |
| HK1219879A1 (zh) * | 2013-06-11 | 2017-04-21 | Bayer Pharma Aktiengesellschaft | 用於治疗癌症的包含mps-1激酶抑制剂和有丝分裂抑制剂的组合 |
| EP2860177A3 (fr) | 2013-09-20 | 2015-06-10 | Bayer Intellectual Property GmbH | Synthèse d'arènes fonctionnalisés |
| CN112778329A (zh) * | 2014-05-19 | 2021-05-11 | Udc 爱尔兰有限责任公司 | 具高效率的荧光有机发光元件 |
| MA41136A (fr) * | 2014-12-09 | 2017-10-17 | Bayer Pharma AG | Composés pour le traitement d'un cancer |
| EP3233127A1 (fr) | 2014-12-15 | 2017-10-25 | Bayer Pharma Aktiengesellschaft | Conjugués anticorps-principe actif (adc) d'inhibiteurs de la ksp ayant des anticorps anti-tweakr aglycosylés |
| CN105985241A (zh) * | 2015-01-27 | 2016-10-05 | 邵阳学院 | α-取代苯乙酸酯类化合物α-糖苷酶抑制作用及其应用 |
| JP6971858B2 (ja) | 2015-06-22 | 2021-11-24 | バイエル ファーマ アクチエンゲゼルシャフト | 酵素開裂性基を有する抗体薬物複合体(adc)および抗体プロドラッグ複合体(apdc) |
| CA2990394A1 (fr) | 2015-06-23 | 2016-12-29 | Bayer Pharma Aktiengesellschaft | Conjugues anticorps-principe actif (adc) d'inhibiteurs de ksp avec des anticorps anti-tweakr |
| WO2017060322A2 (fr) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Conjugué anticorps-médicament (adc) inhibiteur de ptefb |
| EP3919518A1 (fr) | 2016-06-15 | 2021-12-08 | Bayer Pharma Aktiengesellschaft | Conjugués anticorps-médicament spécifiques (adc) avec inhibiteurs de ksp et des anticorps anti-cd123 |
| TW201800408A (zh) | 2016-06-15 | 2018-01-01 | 拜耳製藥公司 | Mps-1抑制劑 |
| WO2018077944A2 (fr) * | 2016-10-27 | 2018-05-03 | Bayer Aktiengesellschaft | 1,2,4-triazolones 4,5-annelées |
| CN110072556B (zh) | 2016-12-21 | 2023-05-02 | 拜耳制药股份公司 | 具有ksp抑制剂的特异性抗体药物缀合物(adc) |
| IL291308B2 (en) | 2016-12-21 | 2024-07-01 | Bayer Pharma AG | Antibody drug conjugates (adcs) having enzymatically cleavable groups |
| CN106831555B (zh) * | 2017-01-22 | 2019-09-24 | 中国农业大学 | 吡啶酰胺类化合物及其制备方法与应用 |
| KR102668688B1 (ko) | 2018-07-23 | 2024-05-24 | 삼성디스플레이 주식회사 | 유기 발광 소자 |
| US12227501B2 (en) | 2019-02-07 | 2025-02-18 | Bayer Aktiengesellschaft | 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as CSNK1 inhibitors |
| KR102661468B1 (ko) | 2019-02-15 | 2024-04-30 | 삼성디스플레이 주식회사 | 유기 발광 소자 및 이를 포함한 전자 장치 |
| KR20210059153A (ko) | 2019-11-14 | 2021-05-25 | 삼성디스플레이 주식회사 | 유기 발광 소자 및 이를 포함한 장치 |
| MX2024010802A (es) * | 2022-03-04 | 2024-09-11 | Sillajen Inc | Combinaciones farmaceuticas para uso en el tratamiento de enfermedades neoplasicas. |
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